PET evaluation of [18F]FCWAY, an analog of the 5-HT1A receptor antagonist, WAY-100635
| Autor: | Margaret G. Der, Lixin Lang, H.Richard Adams, Richard E. Carson, Peter Herscovitch, Elaine M. Jagoda, William C. Eckelman, Hiroshi Watabe |
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| Rok vydání: | 2000 |
| Předmět: |
Fluorine Radioisotopes
Cancer Research medicine.medical_specialty Frontal cortex Pyridines Metabolite Models Biological Piperazines chemistry.chemical_compound Internal medicine medicine Animals Humans Radiology Nuclear Medicine and imaging 5-HT receptor Volume of distribution Chemistry Radiochemistry Antagonist Metabolite analysis Macaca mulatta Endocrinology Receptors Serotonin Molecular Medicine 5-HT1A receptor Serotonin Antagonists Receptors Serotonin 5-HT1 Tomography Emission-Computed |
| Zdroj: | Nuclear Medicine and Biology. 27:493-497 |
| ISSN: | 0969-8051 |
| DOI: | 10.1016/s0969-8051(00)00118-9 |
| Popis: | We synthesized [(18)F]FCWAY, an analog of [carbonyl-(11)C]WAY-100635 ¿[(11)C]N-(2-(1-(4-(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2-(pyridi nyl))cyclohexanecarboxamide¿, by replacing the cyclohexanecarbonyl group acid with a trans-4-fluorocyclohexanecarbonyl group (FC). Control and preblocking studies were performed in anesthetized monkeys. Plasma radioactive metabolite analysis showed the presence of [(18)F]FC and [(18)F]fluoride. Tissue time-radioactivity curves were corrected for metabolite contamination based on separate positron-emission tomography studies of these two labeled metabolites. Analysis using a two-tissue compartment model gave distribution volume (V) estimates (mL/mL) ranging from 33 in frontal cortex to 4 in cerebellum. Preblocking data showed uniform V of 2-3 mL/mL. These studies demonstrate that [(18)F]FCWAY has very similar kinetic characteristics to [(11)C]WAY-100635. |
| Databáze: | OpenAIRE |
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